Abstract
In the last decades, the notion of including excipients in the formulations, as inert substances aiding production processes, has changed and they are recently viewed as multifunctional discrete entities. It is now well documented that excipients serve several roles, spreading from the stabilization and modified release, to providing biocompatible properties and targeting moieties. The aim of this study was to develop matrix-based oral drug delivery systems of bupropion hydrochloride (BUP·HCl) and naltrexone hydrochloride (NTX·HCl), suitable for releasing these active substances in a modified manner, providing a stable level of drug release, which is simultaneously therapeutically effective and non-toxic, thus reducing side effects, after a single dose administration, throughout the gastrointestinal tract. The new formulations, employing hydroxypropylmethycellulose (HPMC K15M) (a cellulosic polymer, which, generally hydrates to form a gelatinous layer that is critical to prevent wetting and rapid drug release from the matrices), poly(methacylic acid-co-ethyl acrylate) 1:1 (Eudragit® L100-55: effective for site specific drug delivery in intestine), poly(ethylene oxide) (PEO) (7 × 106: a high molecular weight polymer, water-soluble, in micro-granular powder form), as the rate controlling polymers, were chosen to lead to a “soothing out” release pattern of these drugs, at 0 ≤ t ≤ 120 min. Moreover, the release of the two drugs from the ulvan-based tablets, was found to follow the desired profile, throughout the entire course of the dissolution experiments.
Highlights
IntroductionThe exact mechanism of action of bupropion hydrochloride (BUP·HCl) remains unclear [5]
Bupropion hydrochloride, (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1propanone, hydrochloride) (BUP·HCl), is a BCS Class I drug [1,2] with a low molecular weight, which has been in therapeutic use, as an antidepressant, since 1989 [3]
The dissolution profiles of both bupropion hydrochloride (BUP·HCl) and naltrexone hydrochloride (NTX·HCl) are depicted in Figures 2 and 3, respectively
Summary
The exact mechanism of action of BUP·HCl remains unclear [5] It was originally classified as an “atypical” antidepressant, due to its different effects, from conventional antidepressants, such as the monoamine oxidase inhibitors, indolamine reuptake (serotonin). It is a potent, non-competitive antagonist of central nicotinic receptors. It was originally classified as an “atypical” antidepressant, due to its different 2 of 18 effects, from conventional antidepressants, such as the monoamine oxidase inhibitors, the tricyclic antidepressants, and the selective serotonin reuptake inhibitors [8]. Liittiesse: xhteyndsrivoxelyybmupertaobpoiolinze, dthinrehou-hmyadnros,xbyybulivperor penioznymaensd(mearyinthlyroC-hYyPd2rBo6x)y, -into three bupropiomn,etwabhoiclhitehsa: vheybderoenxysbuugpgreospteiodnt,othcorenot-rhiybdurteoxaynbdu/oprrobpeiorenspanodnseirbyltehfroo-rhiytsdaronxtiydbeu- propion, pressantwprhoicpherhtiaevs.eHbyeednrosxuygbguepsrtoedpioton caonndtrtihbrueote-haynddr/oxoyrbbueprreosppioonnsaibrelethfoermitasjoarntmidee-pressant tabolitespinrohpuemrtiaens.s,Hwyhdirloextyhbeuepryrothprioo-nhyadnrdotxhyrbeou-phryodpriooxny,bisupforormpieodn ianresmthaellmeraajomr omuentatsbolites in [10]. humans, while the erythro-hydroxybupropion, is formed in smaller amounts [10]
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